Orlistat, a new lipase inhibitor for the management of obesity.

Article Details

Citation

Heck AM, Yanovski JA, Calis KA

Orlistat, a new lipase inhibitor for the management of obesity.

Pharmacotherapy. 2000 Mar;20(3):270-9.

PubMed ID
10730683 [ View in PubMed
]
Abstract

Orlistat, a weight-loss agent with a novel mechanism of action, recently was approved by the Food and Drug Administration for the treatment of obesity. It inhibits gastric and pancreatic lipases in the lumen of the gastrointestinal tract to decrease systemic absorption of dietary fat. In several trials lasting up to 2 years, orlistat was more effective than diet alone for weight reduction and maintenance of lost weight. Orlistat treatment also results in modest improvements in total cholesterol, low-density lipoprotein, blood pressure, and fasting glucose and insulin concentrations. The major adverse effects are gastrointestinal, usually occur early in therapy, and tend to decrease with continued treatment. Because orlistat may decrease the absorption of fat-soluble vitamins, a standard multiple-vitamin supplement is recommended daily during therapy to prevent abnormalities in vitamin serum concentrations. The potential for severe gastrointestinal discomfort and the modest degree of weight loss may limit the agent's clinical utility. Its long-term safety and effectiveness for weight maintenance, cost-effectiveness of treatment, and overall reduction in obesity-related morbidity and mortality remain to be determined.

DrugBank Data that Cites this Article

Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
OrlistatGastric triacylglycerol lipaseProteinHumans
Yes
Inhibitor
Details
OrlistatPancreatic triacylglycerol lipaseProteinHumans
Yes
Inhibitor
Details